One-month release injectable microcapsules of a luteinizing hormone-releasing hormone agonist (leuprolide acetate) for treating experimental endometriosis in rats.
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Injectable microcapsules of leuprolide acetate provided one-month sustained release of the LHRH agonist for treating experimental endometriosis in rats.
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Abstract
Leuprolide acetate is a highly potent analog of luteinizing hormone-releasing hormone. We have prepared 1-month release injectable microcapsules of leuprolide acetate using a biodegradable polymer, poly (dl-lactide-co-glycolide), to treat an endocrine-dependent tumor, prostate cancer. In the present study, the possibility using the microcapsules to treat endometriosis was investigated. In rats, the microcapsules exhibited a pseudo-zero order release from the injection site for 1 month after being administered s.c. and i.m., and maintained effective constant serum levels of the analog during the 4-week treatment. A single injection of the microcapsules (100 micrograms/kg/day as leuprolide acetate) suppressed luteinizing hormone, follicle-stimulating hormone and estradiol for more than 4 weeks, and caused a dramatic regression of growth of Jones experimental endometriosis model in female rats. These results encourage the belief that a 1-month release parenteral preparation of leuprolide acetate may be potentially useful in the therapy of endometriosis in human beings.
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Cited by (12)
- Validation of Rat Endometriosis Model by Using Raloxifene as a Positive Control for the Evaluation of Novel SERM Compounds 2005
- A Prospective Randomized Study Comparing Endocrinological and Clinical Effects of Two Types of GnRH Agonists in Cases of Uterine Leiomyomas or Endometriosis 2000
- Inhibitory effects of a novel aromatase inhibitor, YM511, on growth of endometrial explants and insulin-like growth factor-I gene expression in rats with experimental endometriosis 1997
- Individual and combined effects of triptoreline and gestrinone on experimental endometriosis in rats 1996
- Effects of Gonadotropin‐Releasing Hormone Agonist (GnRHa) and Ovariectomy on Leukocyte Subpopulations in Rats With Autotransplanted Endometrium 1996
- Persistent Suppression of the Pituitary-Gonadal System in Female Rats by Three-Month Depot Injectable Microspheres of Leuprorelin Acetate 1996
- Leukocyte Subpopulation Changes in Rats With Autotransplanted Endometrium and the Effect of Danazol 1995
- Leuprorelin 1994
- Time-related effects of gonadotropin-releasing hormone analog treatment in experimentally induced endometriosis in the rat 1991
- Effects of TAP-144-SR, A Sustained-Release Formulation of a Potent GnRH Agonist, on Experimental Endometriosis in the Rat. 1991
- Effects of danazol, gonadotropin-releasing hormone agonist, and a combination of danazol and gonadotropin-releasing hormone agonist on experimental endometriosis 1990
- Histological Studies on the Therapeutic Effect of Sustained-Release Microspheres of a Potent LHRH Agonist (Leuprorelin Acetate) in an Experimental Endometriosis Model in Rats. 1990
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